pp2a

DT-061, an orally bioavailable protein phosphatase 2A (PP2A) activator, may be used in the therapy of KRAS-mutant and MYC-driven tumorigenesis.

Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride may cause sensitization. Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride promotes apoptosis in HepG2 (IC50= 62 μM) and SK-Hep1 (IC50= 151 μM) cells and inhibits protein phosphatase 2A.

SMAP-2 is an orally bioavailable activator of phosphatase 2A (PP2A) which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A. It inhibits the growth of KRAS-mutant lung cancers .

Calyculin A ((-)-Calyculin A), a toxicant in the Japanese marine sponge CDiscodermia calyxC, is a selective and potent inhibitor of protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A), inducing hyperactivation of cryopreserved bovine spermatozoa and inhibiting radiation-induced gammaH2AX DNA repair disease in human lymphocytes. gammaH2AX DNA repair foci in human lymphocytes.

Okadaic acid is a potent polyether marine toxin that primarily accumulates in the digestive glands of marine mollusks. It is a highly effective and selective inhibitor of protein phosphatases (PPs). By inhibiting these phosphatases, okadaic acid increases the phosphorylation levels of various proteins, acts as a tumor promoter, and induces tau protein phosphorylation. It can be used to establish models of Alzheimer’s disease and skin cancer.

(Rac)-LB-100, a novel Protein Phosphatase 2A (PP2A) inhibitor, sensitizes malignant meningioma cells to the therapeutic effects of radiation

TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.

N-Stearoylsphingosine (Cer(d18:1/18:0)) is an amide compound widely found in eukaryotic organisms that enhances protein phosphatase 2A (PP2A) activity by interfering with the binding of PP2A to PP2A inhibitor 2, leading to dephosphorylation of Akt.N-Stearoylsphingosine is used in prostate cancer research.

LB100 (LB-100) is a water soluble protein phosphatase 2A (PP2A) inhibitor.

D-erythro-Sphingosine (trans-4-Sphingenine) is a protein kinase C (PKC) inhibitor. D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator

Ethoxysanguinarine (6-Ethoxydihydrosanguinarine) shows human blood acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE) inhibitory activity, with IC50 values of 0.83 +/- 0.04 microM and 4.20 +/- 0.19 microM, respectively.

PP2A Cancerous-IN-1 is a potent inhibitor of CIP2A (Cancerous inhibitor of PP2A) and p-Akt, demonstrating significant anti-proliferative effects.

TPP2a is a mitochondrial thioredoxin reductase (TrxR) inhibitor.

Endothall is a protein phosphatase 2A (PP2A) inhibitor, capable of inhibiting PP2A (IC50: 90 nM) and PP1 (IC50: 5 uM). It acts as a herbicide and can also be useful in cancer chemotherapy.

MKI-1 (MASTL Kinase Inhibitor-1) is an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like, IC50= 9.9 μM). MKI-1 exerts radiosensitizer and antitumor activities through PP2A activation in breast cancer.

MP07-66 is a novel FTY720-analog devoid of immunosuppressive effects leads to the reactivation of PP2A, which in turn triggers apoptosis of CLL cells.

(1S,2S,3R)-DT-061, an enantiomer of DT-061, is an orally bioavailable activator of PP2A.

Tautomycin is a potent and specific protein phosphatases 1 and 2A inhibitor (Kiapp of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively), and is an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus.

ATUX-8385 is a potent activator of PP2A. It binds to the PR65 subunit and holds promise for research into cancer and chronic diseases, including Alzheimer's disease and chronic obstructive pulmonary disease (COPD).

1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine (16:1 PE) is a phosphatidylethanolamine that can enhance the activities of PP2A and PTP1B in malignant pleural mesothelioma cells. Additionally, 1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine induces apoptosis in NCI-H28 malignant pleural mesothelioma cells.

Cantharidic acid is a selective inhibitor of protein phosphatase 2 (PP2A) and protein phosphatase 1 (PP1). It impedes cell viability by upregulating the ERK1/2, p38, and JNK1/2 pathways, causes cell cycle arrest at the sub-G1 phase, and induces apoptosis in NPC-39 and HONE-1 cells.

Rubratoxin A is a classical mycotoxin used as a PP2A-specific inhibitor.

FTY720-Mitoxy is an FTY720 analog that can be uesd as a novel stimulator of the activity of the protein phosphatase 2A (PP2A), targeting mitochondria.

TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti-cancer activity while displaying less inhibition of p-EGFR.